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Trabedersen

Names

[ CAS No. ]:
925681-61-4

[ Name ]:
Trabedersen

Biological Activity

[Description]:

Trabedersen (AP 12009) is an antisense oligodeoxynucleotide that specifically inhibits TGF-β2 (TGF-beta/Smad). Trabedersen can be used for the study of malignant brain tumors and other solid tumors overexpressing TGF-β2, such as those of the skin, pancreas and colon[1][2].

[Related Catalog]:

Research Areas >> Cancer
Signaling Pathways >> Stem Cell/Wnt >> TGF-beta/Smad
Signaling Pathways >> TGF-beta/Smad >> TGF-beta/Smad

[In Vitro]

Trabedersen (1-80 μM; 7 days) 减少人胰腺癌细胞系 Hup-T3 中 TGF-β2 的分泌,IC50 在低 μM 范围内,明显抑制细胞增殖,并完全阻断迁移 胰腺癌细胞[2]。 Trabedersen 逆转 TGF-β2 介导的胰腺癌细胞免疫抑制[2]。 Cell Proliferation Assay[2] Cell Line: Hup-T3 cells Concentration: 1 μM, 2.5 μM, 5 μM, 10 μM, 20 μM, 40 μM, 60 μM, 80 μM Incubation Time: 7 days Result: Inhibited cell proliferation, and completely blocked migration of pancreatic cancer cells.

[In Vivo]

Trabedersen(初始负荷剂量为 50 mg/kg ,随后每周 3 次 16 mg/kg;i.p.)可显著降低转移性胰腺癌原位小鼠模型中的肿瘤生长、淋巴结转移和血管生成[2]。 Animal Model: Eight-week-old male athymic nude mice (BALB⁄Cnu ⁄nu) bearing human pancreatic cancer cells[2]. Dosage: Initial loading dose of 50 mg/kg bodyweight followed by 16 mg/kg three times a week. Administration: Intraperitoneal (i.p.) injection; three times a week; for 27 days Result: Significantly reduced tumor growth, lymph node metastasis and angiogenesis.

[References]

[1]. Luc Vallières. Trabedersen, a TGFbeta2-specific antisense oligonucleotide for the treatment of malignant gliomas and other tumors overexpressing TGFbeta2. IDrugs. 2009 Jul;12(7):445-53.  

[2]. Karl-Hermann Schlingensiepen, et al. Transforming growth factor-beta 2 gene silencing with trabedersen (AP 12009) in pancreatic cancer. Cancer Sci. 2011 Jun;102(6):1193-200.  

Chemical & Physical Properties

[ Molecular Weight ]:
5770.75


Related Compounds

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